CA3025253A1 - Derives heterocycliques de prolinamide - Google Patents

Derives heterocycliques de prolinamide Download PDF

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Publication number
CA3025253A1
CA3025253A1 CA3025253A CA3025253A CA3025253A1 CA 3025253 A1 CA3025253 A1 CA 3025253A1 CA 3025253 A CA3025253 A CA 3025253A CA 3025253 A CA3025253 A CA 3025253A CA 3025253 A1 CA3025253 A1 CA 3025253A1
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Prior art keywords
amino
triazol
hydroxypropan
carboxamide
oxoacetyl
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Pending
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CA3025253A
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Inventor
Jinyue DING
Renata Marcella Oballa
David Andrew Powell
Maxim EPIFANOV
Robert Gomez
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Orion Ophthalmology LLC
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Orion Ophthalmology LLC
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Publication of CA3025253A1 publication Critical patent/CA3025253A1/fr
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41921,2,3-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Ophthalmology & Optometry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Management, Administration, Business Operations System, And Electronic Commerce (AREA)

Abstract

L'invention concerne de nouveaux dérivés hétérocycliques de prolinamide de Formule (I), et des sels, solvates, solvates des sels et promédicaments pharmaceutiquement acceptables de ceux-ci, utiles pour prévenir (par ex., retarder l'apparition ou réduire le risque de développer) et traiter (par ex., réguler, soulager ou ralentir l'évolution de) la dégénérescence maculaire liée à l'âge (DMLA) et d'autres maladies associées de l'il. Ces maladies comprennent la DMLA sèche, la DMLA humide, l'atrophie géographique, la rétinopathie diabétique, la rétinopathie du prématuré, la vasculopathie choroïdienne polypoïdale, et la dégénérescence des cellules rétiniennes ou photoréceptrices. L'invention ci-décrite concerne en outre des méthodes destinées à prévenir, ralentir l'évolution de, et traiter la DMLA sèche, la DMLA humide, l'atrophie géographique, la rétinopathie diabétique, la rétinopathie du prématuré, la vasculopathie choroïdienne polypoïdale, et la dégénérescence des cellules rétiniennes ou photoréceptrices, comprenant : l'administration d'une quantité thérapeutiquement efficace du composé selon l'invention. Les composés selon l'invention sont des inhibiteurs de HTRAI. Ainsi, les composés selon l'invention sont utiles pour prévenir et traiter une large gamme de maladies médiées (intégralement ou en partie) par HTRAI. Les composés selon l'invention sont également utiles pour inhiber l'activité de la protéase HTRAI dans l'il ou au locus de l'arthrite ou d'une autre affection associée.
CA3025253A 2016-06-21 2017-06-15 Derives heterocycliques de prolinamide Pending CA3025253A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662352963P 2016-06-21 2016-06-21
US62/352,963 2016-06-21
PCT/US2017/037768 WO2017222915A1 (fr) 2016-06-21 2017-06-15 Dérivés hétérocycliques de prolinamide

Publications (1)

Publication Number Publication Date
CA3025253A1 true CA3025253A1 (fr) 2017-12-28

Family

ID=60783554

Family Applications (1)

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CA3025253A Pending CA3025253A1 (fr) 2016-06-21 2017-06-15 Derives heterocycliques de prolinamide

Country Status (19)

Country Link
US (2) US11377439B2 (fr)
EP (2) EP3472149B1 (fr)
JP (2) JP7179721B2 (fr)
KR (2) KR102595723B1 (fr)
CN (2) CN109476637B (fr)
AU (2) AU2017282651B2 (fr)
BR (1) BR112018076614A2 (fr)
CA (1) CA3025253A1 (fr)
DK (1) DK3472149T3 (fr)
EA (1) EA201990069A1 (fr)
FI (1) FI3472149T3 (fr)
HU (1) HUE064412T2 (fr)
IL (1) IL263284B (fr)
MX (1) MX2018016189A (fr)
PH (1) PH12018502696A1 (fr)
PL (1) PL3472149T3 (fr)
PT (1) PT3472149T (fr)
SG (1) SG11201810848PA (fr)
WO (1) WO2017222915A1 (fr)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109476637B (zh) * 2016-06-21 2022-02-01 奥瑞恩眼科有限责任公司 杂环脯氨酰胺衍生物
US10526315B2 (en) 2016-06-21 2020-01-07 Orion Ophthalmology LLC Carbocyclic prolinamide derivatives

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